An Ethanolic Extract of Boehmeria caudata Aerial Parts Displays Anti-inflammatory and Anti-tumor Activities

Abstract

The tumor microenvironment presents several therapeutic targets, with inflammation being one of them. In search of new drugs, plants have shown to be an effective source of potent anti-inflammatory and anticancer agents. This study aimed to evaluate the antitumoral and inflammatory activities of Boehmeria caudata aerial parts extract. Bioguided in vitro antiproliferative screening showed that phenanthroquinolizidine obtained from the aerial B. caudata ethanolic extract had a straight relationship with activity. Moreover, the orally administered ethanolic extract reduced Ehrlich solid tumor growth and displayed an anti-inflammatory effect in both evaluated experimental models (carrageenan-induced paw edema and croton oil-induced ear edema). These results suggest that the antitumor activity of the ethanolic extract could be explained by antiproliferative effects associated with anti-inflammatory action.

In Silico, In Vitro, and In Vivo Antitumor and Anti-Inflammatory Evaluation of a Standardized Alkaloid-Enriched Fraction Obtained from Boehmeria caudata Sw. Aerial Parts

“…For the in vitro antiproliferative evaluation, the NCI-60 protocol [ 10 ] (with some adaptations) was adopted, expressing the sample activity as the concentration required to elicit total cell growth inhibition (TGI). BcAEF showed, in a first evaluation [ 7 ], a potent growth inhibitor profile against U251 (glioblastoma, TGI < 0.25 µg mL −1 ), MCF-7 (breast, TGI < 0.25 µg mL −1 ) and NCI-H460 (lung, TGI = 0.66 µg mL −1 ) tumor cell lines, similarly to that observed for the ethanolic extract. Herein, using a lower concentration range (0.0025; 0.025; 0.25 and 2.5 μg mL −1 ) and other human tumor cell lines ( Table 1 and Figure S1, Supplementary Material ), BcAEF presented a potent in vitro antiproliferative activity with very low TGI values, although with cytotoxicity against the non-tumor line (HaCat) as well.…”

“…Using acid-base fractionation and liquid-liquid partition with different solvents, BcAEF was produced. By high-resolution electrospray ionization mass spectrometry (HREIMS) and gas chromatography coupled to mass spectrometry (GC-MS), five phenanthroquinolizidine alkaloids (cryptopleurine, boehmeriasin A, boehmeriasin B, julandine, (−)-C(15 R )-hydroxycryptopleurine), one quinolizidine alkaloid [3-(4-hydroxyphenyl)-4-(3-methoxy-4-hydroxyphenyl)-3,4-dehydroquinolizidine], and two acetophenone alkaloids (3,4-dimethoxy-ω-(2′-piperidyl)acetophenone and 2′,4′-dimethoxyacetophenone) were detected in the standardized fraction [ 7 ]. For the in vitro antiproliferative evaluation, the NCI-60 protocol [ 10 ] (with some adaptations) was adopted, expressing the sample activity as the concentration required to elicit total cell growth inhibition (TGI).…”

“…Previously, the in vitro and in vivo activities of the ethanolic extract of Boehmeria caudata aerial parts (BcEE) were reported [ 7 ]. The extract BcEE presented in vitro antiproliferative activity against four human cell lines (one non-tumor and three tumor).…”

“…The extract BcEE presented in vitro antiproliferative activity against four human cell lines (one non-tumor and three tumor). Furthermore, when orally administered, BcEE reduced Ehrlich solid tumor growth with an anti-inflammatory effect, which was evaluated by the carrageenan (CG)-induced paw edema, and croton oil-induced ear edema on mice [ 7 ]. These results suggested that the antitumor activity of the BcEE could be related to the antiproliferative and anti-inflammatory effects, which may have a straight relationship with the phenanthroquinolizidine alkaloids detected in BcEE.…”

“…These results suggested that the antitumor activity of the BcEE could be related to the antiproliferative and anti-inflammatory effects, which may have a straight relationship with the phenanthroquinolizidine alkaloids detected in BcEE. In fact, the alkaloid-enriched fraction of B. caudata (BcAEF) was evaluated in vitro showing an enhanced potency when compared to BcEE [ 7 ]. Continuing the study on the pharmacological profile of B. caudata aerial parts, herein the in silico tubulin interaction (molecular docking studies), in vitro antiproliferative activity (2D model and flow cytometry evaluation), and in vivo antitumor and anti-inflammatory activities of BcAEF are reported for the first time, in order to attest whether the high potency observed in vitro is also maintained in vivo.…”